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地衣酸及其衍生物在药物中的应用:专利研究综述(2000-2017)。

Usnic acid and its derivatives for pharmaceutical use: a patent review (2000-2017).

机构信息

a Department of Medicinal Chemistry, N. N. Vorozhtsov Novosibirsk Institute of Organic Chemistry , Siberian Branch of the Russian Academy of Sciences , Novosibirsk , Russian Federation.

b Novosibirsk State University , Novosibirsk , Russian Federation.

出版信息

Expert Opin Ther Pat. 2018 Jun;28(6):477-491. doi: 10.1080/13543776.2018.1472239. Epub 2018 May 9.

Abstract

INTRODUCTION

Usnic acid (UA) is a lichen-derived secondary metabolite with a unique dibenzofuran skeleton and is commonly found in lichenized fungi of the genera Usnea and Cladonia. Usnic acid has been incorporated for years in cosmetics, perfumery, and traditional medicines. It has a wide range of bioactivities, including antimicrobial, antiviral, anticancer, anti-inflammatory properties.

AREAS COVERED

This review covers patents on therapeutic activities of UA and its synthetic derivatives published during the period 2000-2017.

EXPERT OPINION

UA demonstrates excellent anticancer and antimicrobial properties. However, its application was withdrawn due to acute liver toxicity reported with chronic consumption. The broad spectrum of its biological activity indicates high the variability of UA's binding preferences. The main idea to be addressed in the future should include the synthesis of UA derivatives because these might possess increased bioactivity, bioavailability and decreased toxicity. It is noteworthy that UA derivatives possessed better antibacterial, antitubercular, and anticancer activity than the parent compound . Most importantly, UA and its analogs (to a greater extent than UA) can be useful in cancer drug treatment. They have the potential for joint application with other anticancer drugs in order to overcome drug resistance.

摘要

简介

地衣酸(UA)是一种具有独特二苯并呋喃骨架的衍生次生代谢物,通常存在于地衣真菌属和石松属的真菌中。地衣酸多年来一直被应用于化妆品、香水和传统药物中。它具有广泛的生物活性,包括抗菌、抗病毒、抗癌、抗炎特性。

涵盖领域

本综述涵盖了 2000 年至 2017 年期间发表的关于 UA 及其合成衍生物治疗活性的专利。

专家意见

UA 表现出优异的抗癌和抗菌特性。然而,由于长期食用后报告的急性肝毒性,其应用已被撤回。其广泛的生物活性表明 UA 的结合偏好具有高度可变性。未来应解决的主要问题应包括 UA 衍生物的合成,因为这些衍生物可能具有更高的生物活性、生物利用度和降低的毒性。值得注意的是,UA 衍生物比母体化合物具有更好的抗菌、抗结核和抗癌活性。最重要的是,UA 及其类似物(比 UA 更有优势)可用于癌症药物治疗。它们有可能与其他抗癌药物联合应用,以克服耐药性。

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